<p>Formulation and evaluation of multilamellar vesicles ropivacaine in pain management</p>

Abstract

PurposeThe improvement of postoperative pain control plays an important role in recovery outcomes and patient satisfaction. Multilamellar vesicles ropivacaine, MVR, is being developed to sustain the release of ropivacaine in situ while maintaining the local concentration of ropivacaine within the therapeutic window.MethodsThese studies summarized the processes of MVR formulation development and the evaluation of its releasing profile in vitro and the pharmacokinetics and anesthetic effect in vivo.ResultsThe MVR demonstrates a sustained-release profile in an in vitro serum environment model after 24 hrs of incubation which translates in the in vivo rat pharmacokinetic profile of ropivacaine as a prolonged half-life that is 10-fold longer in duration than plain ropivacaine solution. The anesthetic effect of single-dose MVR is apparent by providing a prolonged analgesia effect compared to plain ropivacaine solution in an in vivo guinea pig pin-prick wheal model after a single intracutaneous injection. From a safety evaluation, MVR is well tolerated after a subcutaneously injection at a dose level of 20 mg/kg in rats, with no observable changes in clinical observation, body weight, organ weight, hematology and serum chemistry analysis.ConclusionThese results suggest that single administration of MVR is a promising candidate in postoperative pain management.

Analgesic effects of different concentrations of ropivacaine in transversalis fascia plane block during laparotomy

“…However, it was found that some patients were predisposed to various adverse reactions after the use of ropivacaine, such as dizziness, tinnitus, nausea and vomiting, and the higher the concentration, the higher the risk of adverse reactions [ 24 ]. The results of this study showed that the number of cases with adverse reactions in the high concentration group was higher than the other two groups, but significant differences were only observed in the comparison with the low concentration group but absent in the comparison with the medium concentration group, which is consistent with the results of Kao Hao-Wen et al [ 25 ], who stated in their article that the incidence of drug side effects of high concentration of ropivacaine was significantly higher than that in low concentration, which was 6.67% ( p < 0.05). It fully illustrates a higher safety profile of medium concentration compared to high concentration ropivacaine.…”

Lipid in Chips: A Brief Review of Liposomes Formation by Microfluidics

“…As a drug delivery system, MLVs and MVVs are more commonly used to achieve long-term drug delivery effects. 48 , 49 To effectively and efficiently function, liposomes need to be prepared at a certain size to allow absorption into cells. Size is a critical parameter in determining liposome drug encapsulation, as well as half-life-in circulation and a smaller liposome diameter, which might be favorable in terms of optimizing in vivo drug release.…”

Local Anesthetics

“…Polymersomes have advances over liposomes with complementary profiles, inspiring the emergence of hybrid carriers [35,36]. Also, multilamellar vesicles with ropivacaine are being investigated to prolong its analgesic effect [37].…”